Pharmacologic Principles Part 1: Pharmaceutics, Pharmacokinetics Flashcards by Shaquan Moore

Study of drugs (pharmacokinetics and pharmacodynamics)

Pharmakon or Pharmacology

Pharmacology

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Comes from Greek word “Pharmakon”

Pharmakon or Pharmacology

Pharmacology

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Means drug(remedy) and poison

Pharmakon or Pharmacology

Pharmakon

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Drug affects the body

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

PHARMACEUTICS

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Body does to the drug

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

PHARMACOKINETICS

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Drug does to the body

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

PHARMACODYNAMICS

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“Peanut Butter”

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

PHARMACOKINETICS

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“Jelly”

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

PHARMACODYNAMICS

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Drug absorption fast to slowest.

a. Enteric Coated Tablets
b. Capsules
c. Oral disintegration, Buccal Tablets, & Oral Soluble Wafers
d. Powder
e. Tablets
f. Liquids, elixers, & syrups
g. Coated Tablets
h. Suspension Solution

c. Oral disintegration, Buccal Tablets, & Oral Soluble Wafers
f. Liquids, elixers, & syrups
h. Suspension Solution
d. Powder
b. Capsules
e. Tablets
g. Coated Tablets
a. Enteric Coated Tablets

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Already in dissolved form and thus absorbed quickly

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Oral Liquids/Suspensions

b. Oral Liquids/Suspensions

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Extra coating on the outside prevents drug from being broken down by the acidic pH of the
stomach

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Enteric Coated Tablets

a. Enteric Coated Tablets

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Drug is not absorbed until they reach the small intestine (higher pH)

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Enteric Coated Tablets

a. Enteric Coated Tablets

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Commonly made to PROTECT the gastric mucosa from irritation

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Enteric Coated Tablets

a. Enteric Coated Tablets

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Release drug over a prolonged period of time

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Extended Release/Sustained Release Tablets

e. Extended Release/Sustained Release Tablets

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◦ Abbreviations => EC

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Enteric Coated Tablets

a. Enteric Coated Tablets

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◦ Abbreviations => SR, SA, CR, XL, XT, ER, and more

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Extended Release/Sustained Release Tablets

e. Extended Release/Sustained Release Tablets

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Sublingual, Buccal

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Oral Mucosa Absorption

d. Oral Mucosa Absorption

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Absorbed through surface of the skin
◦ Skin, Eyes, Ears, Nose, Rectum, Vagina, Lungs and more

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Topical/Transdermal

f. Topical/Transdermal

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IV formulations must have similar pH to blood, otherwise damage can happen to veins/arteries

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Parenteral (Injectable)

c. Parenteral (Injectable)

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◦ Drug is immediately in solution (no need to dissolve)

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Parenteral (Injectable)

c. Parenteral (Injectable)

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◦ Therefore drug is 100% absorbed and ready to work!

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

Parenteral (Injectable)

c. Parenteral (Injectable)

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PHARMACOKINETICS
body does to the drug (ADME)
A-
D-
M-
E-

Absorption
Distribution
Metabolism
Elimination/Excretion

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ADME

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

PHARMACOKINETICS

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Study of what happens to a parent drug from the time it is put into the body until the parent drug and all metabolites have left the body

Nursing process, ADME, QSEN, or IPEC

ADME

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Movement of a drug from its site of administration into the bloodstream for distribution to the tissues Elimination/Excretion Distribution Absorption Metabolism

Absorption

Bioavailability First Pass Effect P-Glycoprotein Routes Elimination/Excretion Distribution Absorption Metabolism

Absorption

Percentage of how much active drug reaches the bloodstream P-Glycoprotein Bioavailability Routes First Pass Effect

Bioavailability

``` Which is true Oral Route is 100% Bioavailable IV Route is 100% Bioavailable Oral Route is variable IV Route is variable ```

IV Route is 100% Bioavailable | Oral Route is variable

What influences bioavailability? a. P-Glycoproteins b. First Pass Effect c. Oral Route/GI Tract factor d. And more! e. None f. All

f. All

First Pass Effect in order a. Metabolized drug reaches general blood circulation b. Drugs can get absorbed in GI tract ▪ gastric mucosa (stomach) ▪ Intestinal mucosa (small intestines) c. The gastric/intestinal mucosal blood flow goes to portal vein d. Swallow the drug orally e. Portal Vein carries the blood to the Liver f. Liver metabolizes drugs (FIRST PASS EFFECT) g. Drug travels down the GI tract

d. Swallow the drug orally g. Drug travels down the GI tract b. Drugs can get absorbed in GI tract ▪ gastric mucosa (stomach) ▪ Intestinal mucosa (small intestines) c. The gastric/intestinal mucosal blood flow goes to portal vein e. Portal Vein carries the blood to the Liver f. Liver metabolizes drugs (FIRST PASS EFFECT) a. Metabolized drug reaches general blood circulation

``` Mouth- Stomach- Small Intestines- Large Intestines- Rectum- ``` Liver or GBC (General Blood Circulation)

``` Mouth- GBC Stomach- Liver Small Intestines- Liver Large Intestines- Liver Rectum- GBC ```

Part of our “defense system” a. P-Glycoproteins b. First Pass Effect c. Oral Route/GI Tract factor d. And more! e. None f. All

a. P-Glycoproteins

Located in essentials areas of body ◦ Blood Brain Barrier, GI Tract a. P-Glycoproteins b. First Pass Effect c. Oral Route/GI Tract factor d. And more! e. None f. All

a. P-Glycoproteins

Called - “Anti-absorption pumps” or Efflux Pumps a. P-Glycoproteins b. First Pass Effect c. Oral Route/GI Tract factor d. And more! e. None f. All

a. P-Glycoproteins

▪P-glycoproteins (More or Less) a. Net Result= More absorption of drugs into the general circulation b. Net Result= Less absorption of drugs into the general circulation

Less b. Net Result= Less absorption of drugs into the general circulation

P-Glycoprotein Inhibitor or Inducer?

Inhibitor

P-Glycoprotein Inhibitor: Cranberry Juice Grape Fruit

Grape Fruit

The drug is absorbed into the systemic circulation through the GI tract Enteral or Parental

Enteral

Oral Sublingual/Buccal Suppositories Enteral or Parental

Enteral

The most common of all routes is the ORAL ROUTE ▪ Most drugs are ABSORBED in stomach or small intestine Enteral or Parental

Enteral

What can influence ORAL route ABSORPTION? a. pH of the GI tract b. Drugs or Meals c. Drug Formulation d. None

a. pH of the GI tract b. Drugs or Meals c. Drug Formulation

◦ Drug is placed under the tongue Buccal or Sublingual

Sublingual

◦ Drug is placed between the cheek and gum Buccal or Sublingual

Buccal

◦ EXAMPLE: NitroSTAT- Nitroglycerin tablets used for acute chest pain (heart attack or angina) Buccal or Sublingual

Sublingual

◦ EXAMPLE: Actiq®- Essentially a fentanyl lollipop for acute, extreme breakthrough cancer pain Buccal or Sublingual

Buccal

Key Points: For Buccal & Sublingual a. Drug is absorbed in the oral mucosa of the mouth and goes directly into the blood stream b. Must allow the drug to dissolve c. Swallowing the medication may inactivate the medication (pH of stomach) d. Do not eat or drink until medication has dissolved e. None f. All

f. All

(Non GI-Tract administration, aka Injections) Enteral or Parental

Parental

◦ The drug is absorbed into the systemic circulation via injections Enteral or Parental

Parental

Intravenous (FASTEST!) Intramuscular/Subcutaneous/Intradermal Epidural- Spinal cord injection Enteral or Parental

Parental

Epidural Enteral or Parental

Parental

Inhalation Topical/Transdermal Instillation (eye/ear/nose drops/sprays) Enteral or Parental

Parental

``` •KEY CONCEPTS 1. Permeability of the Cell Membrane ◦ Lipid Soluble vs Water Soluble ◦ Blood Brain Barrier, Placenta 2. Protein Binding of drugs ◦ Free vs Bound Drug 3. Circulation/Blood Supply ◦ Diseases that alter circulation ``` Which ADME

DISTRIBUTION

▪PERMEABILITY OF CELL MEMBRANE ◦ Easily distribute into fatty tissues where they may store or concentrate Water or Lipid Soluble

Lipid Soluble

▪PERMEABILITY OF CELL MEMBRANE ◦ Have the potential to cross the Blood Brain Barrier (BBB) and the Placenta Water or Lipid Soluble

Lipid Soluble

▪PERMEABILITY OF CELL MEMBRANE ◦ Typically remain in highly vascularized spaces and can easily leave the body via elimination (urine!) Water or Lipid Soluble

Water

▪PROTEIN BINDING ◦ Albumin is the most common blood protein ◦ Some drugs preferentially bind to protein/albumin ◦ Called Highly or Lowly bound drugs“

Highly

Drug is not bound to albumin ◦ can distribute into extravascular tissue to its intended target Bound drug or Free drug

Free drug

Stuck to albumin, stays in the bloodstream ◦ Cannot get to extravascular space and reach intended target Bound drug or Free drug

Bound drug

◦ Free drug Active or Inactive

Active

◦ Bound drug Active or Inactive

Inactive

What are potential complications of Highly Protein Bound Drugs? a. Deficiency in Protein/Albumin b. Competition (two drugs can result in toxicity) c. None d. All

d. All

▪CIRCULATION/BLOOD SUPPLY Vital organs like the heart, kidneys, liver, brain Slow or Rapid

RAPID

▪CIRCULATION/BLOOD SUPPLY Muscle, skin, fat Slow or Rapid

SLOW

▪CIRCULATION/BLOOD SUPPLY CONCERNS/ALTERATIONS a. Diseases/Conditions can alter perfusion b. Peripheral Vascular Disease, Heart Diseases (Heart Failure c. None d. All

d. All

``` Metabolism/Biotransformation Cytochrome P-450 Enzyme Induction Enzyme Inhibition Pro-Drug First Pass Effect ``` Which ADME

Metabolism

BIOTRANSFORMATION = which ADME

Metabolism

The biochemical alteration of a drug (substrate= target drug) Which ADME

Metabolism

(substrate= ?)

target drug

Which of the following are true about metabolism? a. convert drug into an active metabolite or inactive metabolite b. Metabolites could be weaker or stronger than the original drug c. Liver is primary organ d. Minor roles: Skeletal muscle, Kidneys, Lungs, Plasma, Intestinal mucosa e. None f. All

f. All

IMPORTANT REMINDER : NOT ALL DRUGS GO THROUGH METABOLISM True or False

True

Convert drugs to become hydrophilic and polar. P-Glycoproteins or Cytochrome P-450 (CYP450)

Cytochrome P-450 (CYP450)

Liver enzymes target drugs (substrates) P-Glycoproteins or Cytochrome P-450 (CYP450)

Cytochrome P-450 (CYP450)

◦ Typically target drugs that are lipophilic and non polar P-Glycoproteins or Cytochrome P-450 (CYP450)

Cytochrome P-450 (CYP450)

Both Enzyme Induction, Enzyme Inhibition P-Glycoproteins or Cytochrome P-450 (CYP450)

Cytochrome P-450 (CYP450)

Which are METABOLISM ALTERATION a. Other drugs b. Certain Foods (Grape Fruit) c. Smoking/Alcohol d. Patient variables e. Diseases (liver diseases) f. Genetics* g. Age h. None i. All

i. All

METABOLISM ALTERATION Age ◦ Infants have (limited or unlimited) liver enzymes ◦ Geriatric patients may have (less or more) liver enzyme activity

Age ◦ Infants have limited liver enzymes ◦ Geriatric patients may have less liver enzyme activity

Inducers: PS – PORCS or PACMAN loves Grapefruit juice!

PS – PORCS

Inhibitors: PS – PORCS or PACMAN loves Grapefruit juice!

PACMAN loves Grapefruit juice!

Inducers: PS – PORCS ``` P- phenytoin N- non-DHP Calcium Channel Blockers (diltiazem, verapamil) A- amiodarone R- rifampin C- carbamazepine S- St. John’s Wort (OTC herb) P- phenobarbita O- Oxcarbazepine A- azole antifungal (fluconazole, ketoconazole) C- cimetidine (H2RAs) P- protease inhibitor (HIV) M- macrolides (ACE, Azithromycin, Clarithromycin, Erythromycin) S- Smoking G- Grape Juice ```

``` P – phenytoin S – Smoking P – phenobarbital O – Oxcarbazepine R – rifampin C –carbamazepine S – St. John’s Wort (OTC herb) ```

Inhibitors: PACMAN loves Grapefruit juice! ``` P- phenytoin N- non-DHP Calcium Channel Blockers (diltiazem, verapamil) A- amiodarone R- rifampin C- carbamazepine S- St. John’s Wort (OTC herb) P- phenobarbita O- Oxcarbazepine A- azole antifungal (fluconazole, ketoconazole) C- cimetidine (H2RAs) P- protease inhibitor (HIV) M- macrolides (ACE, Azithromycin, Clarithromycin, Erythromycin) S- Smoking G- Grape Juice ```

P – protease inhibitor (HIV) A – azole antifungal (fluconazole, ketoconazole) C – cimetidine (H2RAs) M – macrolides(ACE, Azithromycin, Clarithromycin, Erythromycin) A – amiodarone N – non-DHP Calcium Channel Blockers (diltiazem, verapamil) ♥’s Grapefruit juice

HEPATOCYTES Kidney or Liver

Liver

◦ Metabolism of drugs (CYP enzymes) Kidney or Liver

Liver

◦ Metabolism of hormones Kidney or Liver

Liver

◦ Protein Synthesis and degradation Kidney or Liver

Liver

◦ Coagulation- uses Vitamin K to make clotting factors Kidney or Liver

Liver

◦ Albumin Kidney or Liver

Liver

◦ Glycogen storage (Glycogenesis) Kidney or Liver

Liver

◦ Cholesterol- Lipids + Bile Acid metabolism Kidney or Liver

Liver

▪ Cirrhosis Kidney or Liver

Liver

▪ Hepatotoxicity Kidney or Liver

Liver

▪ DRUGS (Drug Induced Liver Injury- DILI), Alcoholic Liver Disease, Hepatitis, more! Kidney or Liver

Liver

◦ Dark urine- (bilirubin mixes with urine) Kidney or Liver

Liver

Jaundice (yellow eyes, liver no longer filters bilirubin from blood, or can’t conjugate it so it can’t be removed via bile) Kidney or Liver

Liver

Swelling of abdomen (no longer making sufficient albumin) Kidney or Liver

Liver

Bruising/Bleeding (lack of clotting factors) ◦ Fatigue Kidney or Liver

Liver

Ammonia can concentrate (liver normally converts to urea) Kidney or Liver

Liver

◦ Ammonia accumulation- neurological changes- encephalopathy Kidney or Liver

Liver

PHARMACOKINETICS: METABOLISM Kidney or Liver

Liver

PHARMACOKINETICS: ELIMINATION Kidney or Liver

Kidney

Other Mechanisms: ◦ Liver, Breast milk, Sweat, Bowel (biliary excretion, enterohepatic recirculation) METABOLISM or ELIMINATION

ELIMINATION

Injury to the kidney which results in a sudden elevated SCr/BUN and a decreased eGFR/CrCl Chronic Kidney Disease, Acute Kidney Injury, or Nephrotoxicity

Acute Kidney Injury

Chronically elevated SCr/BUN, decreased eGFR/CrCl Chronic Kidney Disease, Acute Kidney Injury, or Nephrotoxicity

Chronic Kidney Disease

Certain drugs may be harmful to the kidneys. We call the resulting damage, nephrotoxicity. Clinically, this is also called an acute kidney injury Chronic Kidney Disease, Acute Kidney Injury, or Nephrotoxicity

Nephrotoxicity